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icatibant 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definition	Drug id	CAS RN
bradykinin receptors antagonists	4186	130308-48-4

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: icatibant accord WIN-65365 WIN 65365 icatibant firazyr icatibant acetate	a potent bradykinin (B2) receptor antagonist; WIN 65365 is an L-Tic(7) stereoisomer Molecular weight: 1304.54 Formula: C59H89N19O13S CLOGP: -3.47 LIPINSKI: 3 HAC: 32 HDO: 18 TPSA: 516.22 ALOGS: -4.56 ROTB: 30

Molecule

Description

Molfile Inchi Smiles

Synonyms:

icatibant accord
WIN-65365
WIN 65365
icatibant
firazyr
icatibant acetate

a potent bradykinin (B2) receptor antagonist; WIN 65365 is an L-Tic(7) stereoisomer

Molecular weight: 1304.54
Formula: C59H89N19O13S
CLOGP: -3.47
LIPINSKI: 3
HAC: 32
HDO: 18
TPSA: 516.22
ALOGS: -4.56
ROTB: 30

Drug dosage:

Dose	Unit	Route
30	mg	P

ADMET properties:

None

Approvals:

Date	Agency	Company
Sept. 21, 2018	PMDA	Shire Japan KK
July 11, 2008	EMA	Shire Pharmaceuticals Ireland Limited
Aug. 25, 2011	FDA	SHIRE ORPHAN THERAP

FDA Adverse Event Reporting System (Female)

MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Hereditary angioedema	2448.29	25.59	448	5643	7114	63475817
Laryngeal oedema	217.83	25.59	59	6032	5659	63477272
Inappropriate schedule of product administration	214.95	25.59	130	5961	103835	63379096
Pharyngeal oedema	213.85	25.59	71	6020	13650	63469281
Prescribed overdose	166.65	25.59	76	6015	34077	63448854
Pharyngeal swelling	140.44	25.59	43	6048	6361	63476570
Product dose omission issue	130.54	25.59	135	5956	234178	63248753
Injection site pain	129.88	25.59	104	5987	129696	63353235
Product availability issue	126.91	25.59	36	6055	4085	63478846
No adverse event	123.77	25.59	66	6025	41339	63441592
Swollen tongue	78.15	25.59	46	6045	34754	63448177
Abdominal distension	77.28	25.59	65	6026	86550	63396381
COVID-19	75.41	25.59	72	6019	113031	63369900
Insurance issue	69.42	25.59	25	6066	6096	63476835
Stress	54.97	25.59	48	6043	67119	63415812
Hospitalisation	54.48	25.59	53	6038	85028	63397903
Injection site erythema	53.61	25.59	52	6039	83122	63399809
Localised oedema	50.06	25.59	19	6072	5359	63477572
Swelling face	47.25	25.59	43	6048	63432	63419499
Device related infection	44.97	25.59	28	6063	23364	63459567
Angioedema	44.82	25.59	37	6054	47928	63435003
Poor venous access	42.53	25.59	23	6068	14762	63468169
Weight decreased	36.13	25.59	81	6010	276717	63206214
Supernumerary teeth	33.01	25.59	4	6087	0	63482931
Nonspecific reaction	32.27	25.59	11	6080	2281	63480650
Injection site swelling	31.11	25.59	30	6061	47542	63435389
Expired product administered	30.87	25.59	14	6077	6167	63476764
COVID-19 immunisation	30.84	25.59	10	6081	1777	63481154
Pregnancy	29.46	25.59	26	6065	36810	63446121
Product distribution issue	28.88	25.59	9	6082	1407	63481524
Weight increased	27.21	25.59	70	6021	260722	63222209
Therapy interrupted	26.14	25.59	23	6068	32432	63450499
Unevaluable event	25.61	25.59	28	6063	51358	63431573

FDA Adverse Event Reporting System (Male)

MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Hereditary angioedema	767.60	40.48	110	1205	937	34954679
Inappropriate schedule of product administration	67.90	40.48	37	1278	62259	34893357
Product availability issue	65.46	40.48	15	1300	1872	34953744
Injection site pain	50.44	40.48	26	1289	38979	34916637
Prescribed overdose	43.50	40.48	16	1299	10631	34944985
Angioedema	42.87	40.48	23	1292	37351	34918265
Weight increased	42.63	40.48	32	1283	93001	34862615
Product dose omission issue	41.63	40.48	35	1280	119676	34835940

FDA Adverse Event Reporting System (Geriatric)

MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Hereditary angioedema	2148.63	27.59	360	4890	4975	79734163
Pharyngeal oedema	195.12	27.59	63	5187	16209	79722929
Inappropriate schedule of product administration	190.49	27.59	115	5135	133513	79605625
Laryngeal oedema	164.08	27.59	47	5203	8082	79731056
Product availability issue	161.87	27.59	40	5210	3907	79735231
Product dose omission issue	149.17	27.59	126	5124	247411	79491727
Injection site pain	143.04	27.59	95	5155	129743	79609395
Prescribed overdose	111.73	27.59	53	5197	37830	79701308
No adverse event	103.49	27.59	50	5200	37142	79701996
COVID-19	80.15	27.59	73	5177	157601	79581537
Localised oedema	64.57	27.59	23	5227	7929	79731209
Weight increased	56.81	27.59	80	5170	277306	79461832
Angioedema	56.79	27.59	44	5206	75991	79663147
Swollen tongue	48.81	27.59	32	5218	42538	79696600
Injection site erythema	47.27	27.59	40	5210	78157	79660981
Expired product administered	44.70	27.59	17	5233	7034	79732104
Insurance issue	44.35	27.59	16	5234	5717	79733421
Body height increased	39.20	27.59	7	5243	138	79739000
Weight decreased	38.42	27.59	77	5173	355121	79384017
Hospitalisation	37.17	27.59	38	5212	94198	79644940
COVID-19 immunisation	36.98	27.59	10	5240	1389	79737749
Stress	36.78	27.59	35	5215	79577	79659561
Pharyngeal swelling	36.30	27.59	15	5235	7704	79731434
Product use issue	33.59	27.59	54	5196	209768	79529370
Pregnancy	27.92	27.59	19	5231	26832	79712306

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

Source	Code	Description
ATC	B06AC02	BLOOD AND BLOOD FORMING ORGANS OTHER HEMATOLOGICAL AGENTS OTHER HEMATOLOGICAL AGENTS Drugs used in hereditary angioedema
MeSH PA	D000700	Analgesics
MeSH PA	D018712	Analgesics, Non-Narcotic
MeSH PA	D000893	Anti-Inflammatory Agents
MeSH PA	D000894	Anti-Inflammatory Agents, Non-Steroidal
MeSH PA	D018501	Antirheumatic Agents
MeSH PA	D065094	Bradykinin B2 Receptor Antagonists
MeSH PA	D065168	Bradykinin Receptor Antagonists
MeSH PA	D051056	Complement Inactivating Agents
MeSH PA	D007155	Immunologic Factors
MeSH PA	D007166	Immunosuppressive Agents
MeSH PA	D018373	Peripheral Nervous System Agents
MeSH PA	D018689	Sensory System Agents
FDA MoA	N0000182964	Bradykinin B2 Receptor Antagonists
FDA EPC	N0000182965	Bradykinin B2 Receptor Antagonist
CHEBI has role	CHEBI:35530	beta-adrenergic blockers
CHEBI has role	CHEBI:63175	peptidomimetics
CHEBI has role	CHEBI:68557	bradykinin receptor antagonists

Drug Use | Suggest Off label Use Form| |View source of the data|

Disease	Relation	SNOMED_ID	DOID
Hereditary angioneurotic edema	indication	82966003	DOID:14735

🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	3.3	acidic
pKa2	13.85	acidic
pKa3	12.18	Basic
pKa4	10.88	Basic
pKa5	10.16	Basic
pKa6	7.56	Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Bioact source	MoA source
B2 bradykinin receptor	GPCR	P30411	BKRB2_HUMAN	ANTAGONIST	Ki	10.22	CHEMBL	CHEMBL
B1 bradykinin receptor	GPCR	P46663	BKRB1_HUMAN	ANTAGONIST	Ki	7	IUPHAR
B2 bradykinin receptor	GPCR		BKRB2_MOUSE	ANTAGONIST	Ki	9.60	IUPHAR
B2 bradykinin receptor	GPCR		BKRB2_RAT		Ki	10.11	CHEMBL
B2 bradykinin receptor	GPCR		BKRB2_CAVPO		Ki	9.96	CHEMBL
B1 bradykinin receptor	GPCR		BKRB1_RAT	ANTAGONIST	Ki	6.40	IUPHAR

External reference:

ID	Source
4031108	VUID
N0000183562	NUI
D04492	KEGG_DRUG
138614-30-9	SECONDARY_CAS_RN
4031108	VANDF
C0246269	UMLSCUI
CHEBI:68556	CHEBI
CHEMBL2028850	ChEMBL_ID
CHEMBL2028852	ChEMBL_ID
DB06196	DRUGBANK_ID
C065679	MESH_SUPPLEMENTAL_RECORD_UI
667	IUPHAR_LIGAND_ID
6922	INN_ID
7PG89G35Q7	UNII
6918173	PUBCHEM_CID
1148138	RXNORM
160761	MMSL
320534	MMSL
d07393	MMSL
012894	NDDF
012895	NDDF
703834005	SNOMEDCT_US
703835006	SNOMEDCT_US
715582002	SNOMEDCT_US

Pharmaceutical products:

Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Icatibant	HUMAN PRESCRIPTION DRUG LABEL	1	0093-3066	INJECTION, SOLUTION	10 mg	SUBCUTANEOUS	ANDA	27 sections
Icatibant	HUMAN PRESCRIPTION DRUG LABEL	1	0093-3066	INJECTION, SOLUTION	10 mg	SUBCUTANEOUS	ANDA	27 sections
Icatibant	HUMAN PRESCRIPTION DRUG LABEL	1	24201-207	INJECTION, SOLUTION	30 mg	SUBCUTANEOUS	ANDA	29 sections
Icatibant	HUMAN PRESCRIPTION DRUG LABEL	1	24201-207	INJECTION, SOLUTION	30 mg	SUBCUTANEOUS	ANDA	29 sections
Icatibant	HUMAN PRESCRIPTION DRUG LABEL	1	24201-207	INJECTION, SOLUTION	30 mg	SUBCUTANEOUS	ANDA	29 sections
Icatibant	HUMAN PRESCRIPTION DRUG LABEL	1	24201-207	INJECTION, SOLUTION	30 mg	SUBCUTANEOUS	ANDA	29 sections
Icatibant	HUMAN PRESCRIPTION DRUG LABEL	1	54092-135	INJECTION, SOLUTION	30 mg	SUBCUTANEOUS	NDA authorized generic	34 sections
Firazyr	HUMAN PRESCRIPTION DRUG LABEL	1	54092-702	INJECTION, SOLUTION	30 mg	SUBCUTANEOUS	NDA	34 sections
Firazyr	HUMAN PRESCRIPTION DRUG LABEL	1	54092-702	INJECTION, SOLUTION	30 mg	SUBCUTANEOUS	NDA	34 sections
Firazyr	HUMAN PRESCRIPTION DRUG LABEL	1	54092-702	INJECTION, SOLUTION	30 mg	SUBCUTANEOUS	NDA	34 sections
Icatibant	Human Prescription Drug Label	1	55150-351	INJECTION, SOLUTION	30 mg	SUBCUTANEOUS	ANDA	28 sections
ICATIBANT	HUMAN PRESCRIPTION DRUG LABEL	1	60505-6214	INJECTION, SOLUTION	30 mg	SUBCUTANEOUS	ANDA	29 sections
ICATIBANT	HUMAN PRESCRIPTION DRUG LABEL	1	60505-6214	INJECTION, SOLUTION	30 mg	SUBCUTANEOUS	ANDA	29 sections
ICATIBANT	HUMAN PRESCRIPTION DRUG LABEL	1	60505-6214	INJECTION, SOLUTION	30 mg	SUBCUTANEOUS	ANDA	29 sections
Icatibant	HUMAN PRESCRIPTION DRUG LABEL	1	63323-574	INJECTION, SOLUTION	10 mg	SUBCUTANEOUS	ANDA	29 sections
Icatibant	HUMAN PRESCRIPTION DRUG LABEL	1	68462-828	INJECTION, SOLUTION	30 mg	SUBCUTANEOUS	ANDA	29 sections
Icatibant	HUMAN PRESCRIPTION DRUG LABEL	1	68462-828	INJECTION, SOLUTION	30 mg	SUBCUTANEOUS	ANDA	29 sections
ICATIBANT	HUMAN PRESCRIPTION DRUG LABEL	1	69097-664	INJECTION	30 mg	SUBCUTANEOUS	ANDA	25 sections
ICATIBANT	HUMAN PRESCRIPTION DRUG LABEL	1	69097-664	INJECTION	30 mg	SUBCUTANEOUS	ANDA	25 sections
SAJAZIR	HUMAN PRESCRIPTION DRUG LABEL	1	70709-013	INJECTION	30 mg	SUBCUTANEOUS	ANDA	25 sections
SAJAZIR	HUMAN PRESCRIPTION DRUG LABEL	1	70709-013	INJECTION	30 mg	SUBCUTANEOUS	ANDA	25 sections
Icatibant	Human Prescription Drug Label	1	71225-114	INJECTION	30 mg	SUBCUTANEOUS	ANDA	26 sections